section name header

Introduction ⬇

AHFS Class:

Generic Name(s):

Telisotuzumab vedotin-tllv, a c-Met-directed antibody conjugated with the microtubule inhibitor monomethyl auristatin E (MMAE), is an antineoplastic agent.1

Uses ⬆ ⬇

Non-small Cell Lung Cancer (NSCLC)

Telisotuzumab vedotin-tllv is used for the treatment of adults with locally advanced or metastatic non-squamous non-small cell lung cancer (NSCLC) with high c-Met protein overexpression (≥50% of tumor cells with strong [3+] staining), as determined by an FDA-approved test, who have received a prior systemic therapy.1

This indication is approved under accelerated approval based on overall response rate (ORR) and duration of response (DOR).1 Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).1

Clinical Experience

Efficacy of telisotuzumab vedotin-tllv was demonstrated in an open-label, single-arm, multi-cohort, phase 2 study (LUMINOSITY; NCT03539536) in adult patients with locally advanced or metastatic epidermal growth factor receptor (EGFR) wild-type non-squamous NSCLC with c-Met protein overexpression who received prior treatment with systemic therapy (including no more than 1 line of prior chemotherapy).1,  2,  3 High c-Met protein overexpression was defined as ≥50% of tumor cells with strong (3+) membrane staining on archival or recent tissue samples by immunohistochemistry and was determined by prospective testing at a central laboratory prior to enrollment.1,  2,  3 Patients who received radiation therapy to the lungs <6 months prior to enrollment and patients with a history of interstitial lung disease or pneumonitis requiring treatment with corticosteroids or occurring within 3 months of the first dose were excluded.1,  2 Patients received telisotuzumab vedotin-tllv 1.9 mg/kg IV every 2 weeks until disease progression or unacceptable toxicity.1,  2 Efficacy was assessed based on overall response rate according to the Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1 by a blinded independent central review committee; duration of response was assessed as a secondary end point.1

The median age of the 84 patients in the efficacy population was 64 years (range: 38-83 years); the majority of patients were male (75%), White (61%), and former smokers (69%).1,  2,  3 Nearly all patients (99%) had stage IV disease, and 19% had previously treated brain metastases.1,  2,  3 Nearly all patients (99%) had an Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1.2,  3 The median number of lines of prior therapies was 1 (range: 1-3); 73% of patients received 1 line, 24% received 2 lines, and 3.6% received 3 lines of prior systemic therapy.1 The majority of patients who received prior therapies had platinum therapy (96%); 82% received immunotherapy, 6% had targeted therapy, and 3.6% had mesenchymal-epithelial transition (MET) tyrosine kinase inhibitor therapy.1,  3 At the time of the initial analysis, the overall response rate was 34.6%; no patients achieved complete response and the median duration of response was 9 months.2 In the follow-up analysis of LUMINOSITY occurring after follow up of approximately 6 months or longer, the overall response rate was 34.5% and the median duration of response was 7.2 months.1,  3

Clinical Perspective

The American Society of Clinical Oncology (ASCO) guidelines on the management of stage IV NSCLC without driver alterations state that telisotuzumab vedotin-tllv is considered a treatment option in patients previously treated with chemotherapy and immunotherapy who have c-Met protein overexpression NSCLC defined as ≥50% of tumor cells with strong (3+) membrane staining on immunohistochemistry.4

Dosage and Administration ⬆ ⬇

General

Pretreatment Screening

Patient Monitoring

Premedication and Prophylaxis

Table 1: Recommended Premedications for Patients Who Experience Infusion-related Reactions to Telisotuzumab Vedotin-tllv1

Medication Class

Drug (Example or Equivalent)

Dose

Route of Administration

Dosing Window Prior to Infusion

H1-receptor Antihistamine

Diphenhydramine

25-50 mg

IV or orally

Administer 30-60 minutes prior to each infusion

H2-receptor Antihistamine

Famotidine

20 mg

IV or orally

Administer 30-60 minutes prior to each infusion

Antipyretic

Acetaminophen

650-1000 mg

IV or orally

Administer 30-60 minutes prior to each infusion

Glucocorticoid

Methylprednisolone

125 mg (or equivalent)

IV

Administer 30-60 minutes prior to each infusion

Dispensing and Administration Precautions

Cautions ⬆ ⬇

Contraindications

Warnings/Precautions

Peripheral Neuropathy

Telisotuzumab vedotin-tllv can cause peripheral neuropathy, including peripheral sensory neuropathy and peripheral motor neuropathy.1

In the safety population of the LUMINOSITY study, peripheral neuropathy occurred in 51% of patients treated with telisotuzumab vedotin-tllv, including Grade 3 in 11% of patients.1 These adverse effects included peripheral sensory neuropathy in 45% of patients and peripheral motor neuropathy in 9% of patients.1 The median time to onset of peripheral neuropathy was 105 days (range: 1-472 days).1 Peripheral neuropathy led to permanent discontinuation of telisotuzumab vedotin-tllv in 13% of patients.1 The median time to onset of peripheral neuropathy leading to treatment discontinuation was 249 days (range: 57-519 days).1 Of the 7 patients with ongoing motor neuropathy as of their last dose of telisotuzumab vedotin-tllv, 6 had persistent Grade 1 or 2 symptoms 30 days after their last dose.1

Monitor patients for signs and symptoms of new or worsening peripheral neuropathy such as hypoesthesia, hyperesthesia, paresthesia, burning sensation, neuropathic pain, or muscle weakness.1 Withhold, reduce the dosage, or permanently discontinue telisotuzumab vedotin-tllv based on severity.1

Interstitial Lung Disease/Pneumonitis

Telisotuzumab vedotin-tllv can cause severe, life-threatening, or fatal interstitial lung disease (ILD)/pneumonitis.1

In the safety population of the LUMINOSITY study, ILD/pneumonitis occurred in 10% of patients treated with telisotuzumab vedotin-tllv, including Grade 3 or Grade 4 in 3% and 0.6% of patients, respectively.1 There were 3 fatal cases of ILD/pneumonitis in patients who received telisotuzumab vedotin-tllv.1 The median time to onset of ILD/pneumonitis was 48 days (range: 23-85 days).1 ILD/pneumonitis led to permanent discontinuation of telisotuzumab vedotin-tllv in 7% of patients.1 The median time to onset of ILD/pneumonitis leading to treatment discontinuation was 46 days (range: 23-85 days).1

Advise patients to immediately report cough, dyspnea, fever, and/or any new or worsening respiratory symptoms.1 Monitor patients for signs and symptoms of ILD/pneumonitis.1 Withhold or permanently discontinue telisotuzumab vedotin-tllv based on severity.1

Ocular Surface Disorders

Telisotuzumab vedotin-tllv can cause ocular surface disorders including blurred vision, visual impairment, keratitis, and dry eye.1

In the safety population of the LUMINOSITY study, ocular surface disorders occurred in 25% of patients treated with telisotuzumab vedotin-tllv.1 The most common ocular surface disorders were blurred vision (15%), keratitis (11%), and dry eye (5%).1 Grade 3 ocular surface disorders occurred in 1.2% of patients (blurred vision [1.2%] and keratitis [0.6%]).1 The median time to onset of ocular surface disorders was 47 days (range: 1-319 days).1

Monitor patients for ocular surface disorders during treatment with telisotuzumab vedotin-tllv.1 Withhold telisotuzumab vedotin-tllv and refer patients who develop Grade ≥2 ocular toxicity to an eye care professional for an ophthalmic examination and treatment.1 Withhold or permanently discontinue telisotuzumab vedotin-tllv based on severity.1

Infusion-related Reactions

Telisotuzumab vedotin-tllv can cause infusion-related reactions.1 Signs and symptoms of infusion-related reactions include dyspnea, flushing, chills, nausea, chest discomfort, and hypotension.1 The median time to onset of infusion-related reactions was 28 days (range: 1-43 days).1

In the safety population of the LUMINOSITY study, infusion-related reactions occurred in 3% of patients treated with telisotuzumab vedotin-tllv including Grade 3 in 1.2% and Grade 4 in 0.6%.1 Infusion-related reactions led to permanent discontinuation of telisotuzumab vedotin-tllv in 0.6% of patients.1

Monitor patients for signs and symptoms of infusion reactions during telisotuzumab vedotin-tllv treatment.1 Withhold, reduce the rate of infusion, or permanently discontinue telisotuzumab vedotin-tllv based on severity.1 For patients who experience infusion-related reactions, administer premedications prior to subsequent infusions.1

Embryo-fetal Toxicity

Based on the mechanism of action and findings in animals, telisotuzumab vedotin-tllv can cause fetal harm when administered to a pregnant woman.1 The small molecule component of telisotuzumab vedotin-tllv, monomethyl auristatin E (MMAE), caused adverse developmental outcomes in rats, including embryo-fetal mortality and structural abnormalities, at exposures similar to those occurring clinically at the recommended dose.1

Advise patients of the potential risk to a fetus.1 Advise females of reproductive potential to use effective contraception during treatment with telisotuzumab vedotin-tllv and for 2 months after the last dose.1 Advise male patients with female partners of reproductive potential to use effective contraception during treatment with telisotuzumab vedotin-tllv and for 4 months after the last dose.1

Immunogenicity

Following administration of telisotuzumab vedotin-tllv in a clinical study, 60 of 269 patients (22%) tested positive for treatment-emergent antibodies at one or more post-baseline time points.1 Of those who tested positive for anti-drug antibody, neutralizing antibodies were detected in 23 of the 60 patients (38%).1 Development of anti-drug and neutralizing antibodies resulted in a 17% decrease in clearance of telisotuzumab vedotin-tllv.1 There are insufficient data to assess whether the observed anti-drug antibody-associated changes in pharmacokinetics affect the safety and efficacy of telisotuzumab vedotin-tllv.1

Specific Populations

Pregnancy

There are no available human data on telisotuzumab vedotin-tllv use in pregnant women to inform a drug-associated risk.1 Based on the mechanism of action and findings in animals, telisotuzumab vedotin-tllv can cause fetal harm when administered to a pregnant woman.1 In an animal reproduction study, administration of the small molecule component of telisotuzumab vedotin-tllv, MMAE, to pregnant rats during organogenesis resulted in embryo-fetal mortality and structural abnormalities at exposures similar to the clinical exposure at the recommended dose.1 Advise patients of the potential risks to a fetus.1

Lactation

There are no data on the presence of telisotuzumab vedotin-tllv or MMAE in human milk, the effects on the breast-fed child, or the effects on milk production.1 Because of the potential for serious adverse effects in a breast-fed child, advise lactating women not to breast-feed during treatment with telisotuzumab vedotin-tllv and for 1 month after the last dose.1

Females and Males of Reproductive Potential

Telisotuzumab vedotin-tllv can cause fetal harm when administered to a pregnant woman.1,  1 Advise females of reproductive potential to use effective contraception during treatment with telisotuzumab vedotin-tllv and for 2 months after the last dose.1 Based on genotoxicity findings, advise male patients with female partners of reproductive potential to use effective contraception during treatment with telisotuzumab vedotin-tllv and for 4 months after the last dose.1

Based on findings in animal studies with MMAE-containing antibody-drug conjugates, telisotuzumab vedotin-tllv may impair female fertility.1 The effect on fertility is reversible.1 Based on findings from animal studies, telisotuzumab vedotin-tllv may impair male fertility.1 The reversibility of this effect is unknown.1

Pediatric Use

Safety and effectiveness of telisotuzumab vedotin-tllv have not been established in pediatric patients.1

Geriatric Use

Of the 168 patients with previously treated epidermal growth factor receptor wild-type non-squamous NSCLC with c-Met protein overexpression treated with telisotuzumab vedotin-tllv, 50% were ≥65 years of age and 12% were ≥75 years of age.1 No overall differences in safety or effectiveness were observed between older and younger patients.1

Hepatic Impairment

Telisotuzumab vedotin-tllv has not been studied in patients with moderate or severe hepatic impairment.1 Patients with moderate or severe hepatic impairment are likely to have increased exposure to MMAE, which may increase the risk of adverse effects.1 Avoid use of telisotuzumab vedotin-tllv in patients with moderate or severe hepatic impairment (total bilirubin concentration exceeding 1.5 times the upper limit of normal [ULN] with any AST concentration).1 No significant differences in the pharmacokinetics of telisotuzumab vedotin-tllv or unconjugated MMAE were observed in patients with mild hepatic impairment (total bilirubin concentration not exceeding the ULN with AST concentration exceeding the ULN, or total bilirubin concentration exceeding but no more than 1.5 times the ULN with any AST concentration).1

Renal Impairment

No clinically important differences in the pharmacokinetics of telisotuzumab vedotin-tllv or unconjugated MMAE were observed in patients with mild or moderate (creatinine clearance 30-89 mL/minute) renal impairment.1 The effect of severe (creatinine clearance <30 mL/minute) renal impairment or end-stage renal disease with or without dialysis on the pharmacokinetics of telisotuzumab vedotin-tllv or unconjugated MMAE is unknown.1

Common Adverse Effects

The most common adverse effects of telisotuzumab vedotin-tllv (≥20% of patients) are peripheral neuropathy, fatigue, decreased appetite, and peripheral edema.1

The most common Grade 3 or 4 laboratory abnormalities (≥2%) are decreased lymphocytes, increased glucose, increased ALT, increased gamma-glutamyl transferase, decreased phosphorus, decreased sodium, decreased hemoglobin, and decreased calcium.1

Drug Interactions ⬆ ⬇

Telisotuzumab vedotin-tllv metabolism has not been evaluated.1 The small molecule, monomethyl auristatin E (MMAE), is a substrate of cytochrome P-450 (CYP) 3A4/5 and P-glycoprotein (P-gp) and is an inhibitor of CYP3A4/5.1

No clinical studies have evaluated the potential for drug-drug interactions with telisotuzumab vedotin-tllv.1

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Concomitant use of telisotuzumab vedotin-tllv with strong CYP3A inhibitors may increase unconjugated MMAE exposure, which may increase the risk of adverse effects of telisotuzumab vedotin-tllv.1 Monitor patients for adverse effects of telisotuzumab vedotin-tllv when used concomitantly with strong CYP3A inhibitors.1

The AUC of MMAE is predicted to increase by 1.4-fold following concomitant administration of telisotuzumab vedotin-tllv with ketoconazole, a strong CYP3A inhibitor.1,  6

The AUC of MMAE is predicted to decrease by 70% following concomitant administration of telisotuzumab vedotin-tllv with rifampin, a strong CYP3A inducer.1,  6

No clinically important difference in the pharmacokinetics of midazolam, a sensitive CYP3A substrate, are predicted when used concomitantly with telisotuzumab vedotin-tllv.1,  6

Other Information ⬆ ⬇

Description

Telisotuzumab vedotin-tllv is a c-Met-directed antibody drug conjugate (ADC).1 The antibody is a humanized immune globulin G1 kappa (IgG1κ) directed against c-Met, the cell surface receptor for hepatocyte growth factor.1 The small molecule, monomethyl auristatin E (MMAE), is a microtubule-disrupting agent, attached to the antibody via a protease-cleavable linker.1 Following binding to c-Met-expressing cells, telisotuzumab vedotin-tllv undergoes internalization and intracellular cleavage of MMAE.1 MMAE disrupts the microtubule network of actively dividing cells, subsequently inducing cell cycle arrest and apoptotic cell death.1 Telisotuzumab vedotin-tllv exhibited antitumor activity in xenograft models of non-small cell lung cancer (NSCLC).1

Telisotuzumab vedotin-tllv and unconjugated MMAE plasma exposure increase proportionally over the dosage range from 1.2-3.3 mg/kg; minimal accumulation occurs.1 The time to maximum plasma concentration of telisotuzumab vedotin-tllv occurs at the end of the infusion, while the time to maximum plasma concentration of MMAE occurs approximately 5 days after administration.1 Plasma protein binding of MMAE ranges from 68-82%.1 The estimated half-life of telisotuzumab vedotin-tllv and MMAE are 3 and 4 days, respectively.1 The metabolism of telisotuzumab vedotin-tllv has not been evaluated.1 It is expected to undergo catabolism to small peptides, amino acids, unconjugated MMAE, and unconjugated MMAE-related catabolites; MMAE is metabolized primarily by cytochrome P-450 3A4.1 No clinically important differences in the pharmacokinetics of telisotuzumab vedotin-tllv or unconjugated MMAE were observed based on age (range: 30-87 years), sex, race, body weight (range: 35-144 kg), mild or moderate (creatinine clearance 30-89 mL/minute) renal impairment, or mild hepatic impairment (total bilirubin concentration not exceeding the upper limit of normal [ULN] with AST concentration exceeding the ULN, or total bilirubin concentration exceeding but no more than 1.5 times the ULN with any AST concentration).1 The effect of severe (creatinine clearance <30 mL/minute) renal impairment, end-stage renal disease with or without dialysis, or moderate to severe hepatic impairment (total bilirubin concentration exceeding 1.5 times the ULN with any AST concentration) on the pharmacokinetics of telisotuzumab vedotin-tllv or unconjugated MMAE are not known.1

Advice to Patients

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations ⬆ ⬇

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Telisotuzumab vedotin-tllv is available only from designated specialty distributors. Contact manufacturer or consult the [Web] website for specific availability information.

Telisotuzumab Vedotin-tllv

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

For injection, for IV infusion

20 mg

Emrelis®

AbbVie

100 mg

Emrelis®

AbbVie

Copyright ⬆ ⬇

AHFS® Drug Information. © Copyright, 1959-2026, Selected Revisions October 10, 2026. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.

References ⬆

Only references cited for selected revisions after 1984 are available electronically.

1. AbbVie Inc. Emrelis® (telisotuzumab vedotin-tllv) injection for intravenous infusion prescribing information. North Chicago, IL; 2025 May.

2. Camidge DR, Bar J, Horinouchi H, et al. Telisotuzumab vedotin monotherapy in patients with previously treated c-Met protein-overexpressing advanced nonsquamous EGFR -wildtype non-small cell lung cancer in the phase II LUMINOSITY trial. J Clin Oncol . 2024; 42(25):3000-3011.

3. Girard N, Goldman J, Lu S, et al. Telisotuzumab vedotin monotherapy in patients with previously treated c-Met protein overexpressing, nonsquamous, EGFR wild-type advanced NSCLC: updated analysis of the LUMINOSITY trial. JTO Clin Res Rep . 2026;7(7):100988.

4. Bazhenova L, Ismaila N, Durm G, et al. Therapy for stage IV non-small cell lung cancer without driver alterations: ASCO living guideline, 2026.3.1. J Clin Oncol . 2026;44(18):e101-e112.

5. Institute for Safe Medication Practices (ISMP). ISMP list of high-alert medications in acute care settings (2024). Accessed 2026 Jul 12. [Web]

6. Riad MMH, Brunsdon P, Menon R, et al. Assessment of telisotuzumab vedotin drug-drug interaction potential using physiologically-based pharmacokinetic modeling and simulations. J Clin Pharmacol . 2025;65(12):1732-1745.